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Avacopan (CCX168) is a first-in-class, potent, selective and orally available complement 5a receptor (C5aR1 or CD88) antagonist with an IC50 of 0.1 nM.
Avacopan (CCX168) blocked the C5a binding, C5a-mediated migration, calcium mobilization, and CD11b upregulation in U937 cells as well as in freshly isolated human neutrophils. Avacopan competitively and selectively blocked C5a-induced calcium mobilization in purified human neutrophils, with an IC50 value of 0.2 nM.
In vivo, in mice dosed orally with 0.03 mg/kg of CCX168, the resulting plasma CCX168 concentration of 15 nM (8.7 ng/mL) reduces the drop in circulating leukocytes from 53% to 25%. In mice administered 0.3 mg/kg of CCX168, the resulting plasma CCX168 concentration of 75 nM (44 ng/mL) reduces the drop in circulating leukocytes from 53% to only 10% relative to baseline (p<0.05 for CCX168 vs. vehicle control). Oral doses of CCX168 of either 3 or 30 mg/kg completely blocks C5a-induced leukopenia in hC5aR knock-in mice.
Exp Ther Med. 2022 Jun 7;24(2):493.
The complement C3a-C3aR and C5a-C5aR pathways promote viability and inflammation of human retinal pigment epithelium cells by targeting NF-κB signaling
Avacopan purchased from AbMole
| Molecular Weight | 581.64 |
| Formula | C33H35F4N3O2 |
| CAS Number | 1346623-17-3 |
| Solubility (25°C) | DMSO ≥ 9 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Xiao H, et al. J Am Soc Nephrol. C5a receptor (CD88) blockade protects against MPO-ANCA GN.
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